Strategies were developed to design novel, potent, selective, long-duration and centrally active therapeutics for the treatment of (i) Alzheimer's disease and age associated memory deficit, (ii) cancers of the brain, lymphatics, breast and ovaries, (iii) and (iii) drug abuse. Centrally active acetylcholinesterase inhibitors were developed as cognitive enhancers and modulators of beta-amyloid production and are being developed towards the clinical arena for Alzheimer disease. Lipophilic anticancer alkylating agents were developed for cancer treatment, inhibitors of dopamine reuptake and of butyrylcholinesterase are being developed for drug abuse.